LY2874455 potently inhibits FGFR gatekeeper mutants and overcomes mutation-based resistance

The chemical compound LY2874455 has the potential to overcome drug resistance driven by FGFR gatekeeper mutations. X-ray crystallographic studies provide the structural explanation for why this compound is effective against the FGFR gatekeeper mutations.

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Bibliographische Detailangaben
Veröffentlicht in:	Chemical communications (Cambridge, England) England), 2018-10, Vol.54 (85), p.12089-12092
Hauptverfasser:	Wu, Daichao, Guo, Ming, Min, Xiaoli, Dai, Shuyan, Li, Meixiang, Tan, Sijie, Li, Guoqing, Chen, Xiaojuan, Ma, Yao, Li, Jun, Jiang, Longying, Qu, Lingzhi, Zhou, Zhan, Chen, Zhuchu, Chen, Lin, Xu, Guangyu, Chen, Yongheng
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding Sites Cell Line Chemical compounds Crystallography Drug Resistance, Neoplasm - drug effects Humans Imidazoles - pharmacology Indazoles - chemistry Indazoles - pharmacology Mice Mutation Organic chemistry Protein Kinase Inhibitors - pharmacology Pyridazines - pharmacology Receptors, Fibroblast Growth Factor - antagonists & inhibitors Receptors, Fibroblast Growth Factor - chemistry Receptors, Fibroblast Growth Factor - genetics
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Beschreibung
Zusammenfassung:	The chemical compound LY2874455 has the potential to overcome drug resistance driven by FGFR gatekeeper mutations. X-ray crystallographic studies provide the structural explanation for why this compound is effective against the FGFR gatekeeper mutations.
ISSN:	1359-7345 1364-548X
DOI:	10.1039/c8cc07546h